title: Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened.
authors.affiliation: Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA. stefan.peukert@novartis.com.
authors.forename: Stefan
authors.initials: S
authors.lastname: Peukert
authors.forename: Feng
authors.initials: F
authors.lastname: He
authors.forename: Miao
authors.initials: M
authors.lastname: Dai
authors.forename: Rui
authors.initials: R
authors.lastname: Zhang
authors.forename: Yingchuan
authors.initials: Y
authors.lastname: Sun
authors.forename: Karen
authors.initials: K
authors.lastname: Miller-Moslin
authors.forename: Michael
authors.initials: M
authors.lastname: McEwan
authors.forename: Bharat
authors.initials: B
authors.lastname: Lagu
authors.forename: Kate
authors.initials: K
authors.lastname: Wang
authors.forename: Naeem
authors.initials: N
authors.lastname: Yusuff
authors.forename: Aaron
authors.initials: A
authors.lastname: Bourret
authors.forename: Arun
authors.initials: A
authors.lastname: Ramamurthy
authors.forename: Wieslawa
authors.initials: W
authors.lastname: Maniara
authors.forename: Adam
authors.initials: A
authors.lastname: Amaral
authors.forename: Anthony
authors.initials: A
authors.lastname: Vattay
authors.forename: Anlai
authors.initials: A
authors.lastname: Wang
authors.forename: Ribo
authors.initials: R
authors.lastname: Guo
authors.forename: Jing
authors.initials: J
authors.lastname: Yuan
authors.forename: John
authors.initials: J
authors.lastname: Green
authors.forename: Juliet
authors.initials: J
authors.lastname: Williams
authors.forename: Silvia
authors.initials: S
authors.lastname: Buonamici
authors.forename: Joseph F
authors.initials: JF
authors.lastname: Kelleher
authors.forename: Marion
authors.initials: M
authors.lastname: Dorsch
mesh_terms: D000818:Animals; D002460:Cell Line; D004195:Disease Models, Animal; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D051379:Mice; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D000072086:Smoothened Receptor; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C586455:NVP-LEQ506; D011719:Pyrazines; D011724:Pyridazines; D043562:Receptors, G-Protein-Coupled; C491023:SMO protein, human; D000072086:Smoothened Receptor
keywords: antitumor agents; hedgehog signaling; medicinal chemistry; pyridazines; smoothened inhibitors